title: An efficient and expedient method for the synthesis of 11C-labeled α-aminoisobutyric acid: a tumor imaging agent potentially useful for cancer diagnosis.
abstract: We describe the synthesis of (11)C-labeled α-aminoisobutyric acid 2 from iodo[(11)C]methane and methyl N-(diphenylmethylen)-d,l-alaniate (5). The tetrabutylammonium fluoride (TBAF)-promoted α-[(11)C]methylation of sterically hindered analog 5 was a key step in our synthesis process. Total radiochemical conversion of 2 was high and a remote-controlled synthesis was carried out. A comparative tumor positron emission tomography (PET) imaging study using the same model mouse showed higher uptake of 2 than with (11)C-labeled methionine and [(18)F] fluorodeoxyglucose (FDG).
authors.affiliation: Department of Molecular Probes, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan. katok@nirs.go.jp
authors.forename: Koichi
authors.initials: K
authors.lastname: Kato
authors.forename: Atsushi B
authors.initials: AB
authors.lastname: Tsuji
authors.forename: Tsuneo
authors.initials: T
authors.lastname: Saga
authors.forename: Ming-Rong
authors.initials: MR
authors.lastname: Zhang
mesh_terms: D000621:Aminoisobutyric Acids / Q000138:chemical synthesis / Q000737:chemistry*; D000818:Animals; D002250:Carbon Radioisotopes / Q000737:chemistry; D004195:Disease Models, Animal; D051379:Mice; D009369:Neoplasms / Q000000981:diagnostic imaging*; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D000621:Aminoisobutyric Acids; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; C100049:2-aminoisobutyric acid